MA38668B2 - Cristal stabilisé de chlorhydrate de tipiracil, et son procédé de cristallisation - Google Patents
Cristal stabilisé de chlorhydrate de tipiracil, et son procédé de cristallisationInfo
- Publication number
- MA38668B2 MA38668B2 MA38668A MA38668A MA38668B2 MA 38668 B2 MA38668 B2 MA 38668B2 MA 38668 A MA38668 A MA 38668A MA 38668 A MA38668 A MA 38668A MA 38668 B2 MA38668 B2 MA 38668B2
- Authority
- MA
- Morocco
- Prior art keywords
- crystal
- crystallization process
- tipiracil hydrochloride
- stabilized crystal
- stabilized
- Prior art date
Links
- 239000013078 crystal Substances 0.000 title abstract 4
- KGHYQYACJRXCAT-UHFFFAOYSA-N tipiracil hydrochloride Chemical compound Cl.N1C(=O)NC(=O)C(Cl)=C1CN1C(=N)CCC1 KGHYQYACJRXCAT-UHFFFAOYSA-N 0.000 title abstract 3
- 238000002425 crystallisation Methods 0.000 title 1
- 230000008025 crystallization Effects 0.000 title 1
- 238000000034 method Methods 0.000 title 1
- 229960001740 tipiracil hydrochloride Drugs 0.000 title 1
- 238000000634 powder X-ray diffraction Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
- A61K31/7072—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K35/00—Medicinal preparations containing materials or reaction products thereof with undetermined constitution
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Saccharide Compounds (AREA)
Abstract
La présente invention aborde le problème de production d'un cristal stabilisé de monochlorhydrate de 5-chloro-6-[(2-iminopyrrolidin-1-yl)méthyl]- pyrimidine-2,4(1h,3h)-dione. Comme moyen pour résoudre le problème, il est proposé un cristal de monochlorhydrate de 5-chloro-6-[(2-iminopyrrolidin- 1-yl)méthyl]pyrimidine-2,4(1h,3h)-dione. Le cristal présente des pics caractéristiques à des angles de diffraction (2? ± 0,1°) de 11,6°, 17,2°, 17,8°, 23,3°, 27,1° et 29,3° dans la diffraction des rayons x sur poudre.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2013126567 | 2013-06-17 | ||
| PCT/JP2014/065985 WO2014203877A1 (fr) | 2013-06-17 | 2014-06-17 | Cristal stabilisé de chlorhydrate de tipiracil, et son procédé de cristallisation |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MA38668A1 MA38668A1 (fr) | 2018-05-31 |
| MA38668B2 true MA38668B2 (fr) | 2019-09-30 |
Family
ID=52104609
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MA38668A MA38668B2 (fr) | 2013-06-17 | 2014-06-17 | Cristal stabilisé de chlorhydrate de tipiracil, et son procédé de cristallisation |
Country Status (30)
| Country | Link |
|---|---|
| US (3) | US9527833B2 (fr) |
| EP (2) | EP3012255B1 (fr) |
| JP (2) | JP6364409B2 (fr) |
| KR (1) | KR101806346B1 (fr) |
| CN (4) | CN104395307A (fr) |
| AU (2) | AU2014282281C1 (fr) |
| BR (1) | BR112015031619B1 (fr) |
| CA (2) | CA2985006C (fr) |
| CY (1) | CY1124868T1 (fr) |
| DK (1) | DK3012255T3 (fr) |
| ES (1) | ES2898408T3 (fr) |
| GE (2) | GEP20186875B (fr) |
| HK (1) | HK1203071A1 (fr) |
| HR (1) | HRP20211903T1 (fr) |
| HU (1) | HUE057352T2 (fr) |
| LT (1) | LT3012255T (fr) |
| MA (1) | MA38668B2 (fr) |
| MX (1) | MX2015016986A (fr) |
| MY (1) | MY173410A (fr) |
| NZ (1) | NZ714090A (fr) |
| PH (1) | PH12015502809A1 (fr) |
| PL (1) | PL3012255T3 (fr) |
| PT (1) | PT3012255T (fr) |
| RS (1) | RS62691B1 (fr) |
| RU (2) | RU2674441C1 (fr) |
| SG (4) | SG11201509189SA (fr) |
| SI (1) | SI3012255T1 (fr) |
| TW (1) | TWI639592B (fr) |
| UA (1) | UA112626C2 (fr) |
| WO (1) | WO2014203877A1 (fr) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104395307A (zh) | 2013-06-17 | 2015-03-04 | 大鹏药品工业株式会社 | 地匹福林盐酸盐的稳定型晶体及其结晶化方法 |
| CN104744443A (zh) * | 2013-12-26 | 2015-07-01 | 江苏豪森药业股份有限公司 | 嘧啶二酮类化合物盐酸盐新晶型及其制备方法 |
| CN103788075B (zh) * | 2014-02-19 | 2018-03-27 | 齐鲁制药有限公司 | 一种胸苷磷酸化酶抑制剂的结晶形式及其制备方法 |
| CN104945385A (zh) * | 2014-03-31 | 2015-09-30 | 江苏豪森药业股份有限公司 | Tipracil盐酸盐的新晶型及其制备方法 |
| CN106018573B (zh) * | 2016-03-16 | 2018-09-18 | 江苏悦兴药业有限公司 | 一种tas-102中盐酸替比拉西的纯度检测方法 |
| CN105859691A (zh) * | 2016-04-07 | 2016-08-17 | 扬子江药业集团南京海陵药业有限公司 | 一种胸苷磷酸化酶抑制剂的新型结晶形式及其制备方法 |
| WO2018039359A1 (fr) * | 2016-08-23 | 2018-03-01 | Board Of Regents, The University Of Texas System | Procédés de traitement d'une maladie osseuse associée à un cancer. |
| WO2019002407A1 (fr) * | 2017-06-28 | 2019-01-03 | Amneal Pharmaceuticals Company Gmbh | Procédé de préparation de tipiracil chlorhydrate |
| CN107216314A (zh) * | 2017-08-02 | 2017-09-29 | 国药心制药有限公司 | 一种盐酸替匹嘧啶的晶型及其制备方法 |
| WO2019049174A1 (fr) * | 2017-09-07 | 2019-03-14 | Msn Laboratories Private Limited, R&D Center | Formes à l'état solide de chlorhydrate de 5-chloro-6-[(2-iminopyrrolidin-1-yl)méthyl]pyrimidine-2,4-(1h,3h)-dione et procédés de préparation associés |
| WO2019053574A1 (fr) * | 2017-09-14 | 2019-03-21 | Aurobindo Pharma Limited | Procédé de préparation de chlorhydrate de tipiracil cristallin |
| JP7330180B2 (ja) * | 2017-11-02 | 2023-08-21 | プロコス ソシエタ ペル アチオニ | チピラシル塩酸塩結晶ｉｉｉ型の製造方法 |
| US11730753B2 (en) | 2018-03-03 | 2023-08-22 | Natco Pharma Limited | Stable pharmaceutical compositions comprising trifluridine and tipiracil hydrochloride |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP3088757B2 (ja) | 1995-03-29 | 2000-09-18 | 大鵬薬品工業株式会社 | ウラシル誘導体並びにそれを含有する抗腫瘍効果増強剤及び抗腫瘍剤 |
| EP0884051B1 (fr) | 1996-09-24 | 2004-12-15 | Taiho Pharmaceutical Company Limited | Inhibiteurs de metastases cancereuses contenant des derives d'uracile |
| JP4049477B2 (ja) | 1999-03-23 | 2008-02-20 | 大鵬薬品工業株式会社 | 副作用軽減剤 |
| JP4110347B2 (ja) | 1999-11-05 | 2008-07-02 | 大鵬薬品工業株式会社 | 抗ｈｉｖ剤 |
| US7799783B2 (en) * | 2005-01-26 | 2010-09-21 | Taiho Pharmaceutical Co., Ltd. | Method of administrating an anticancer drug containing α, α, α-trifluorothymidine and thymidine phosphorylase inhibitor |
| KR101390144B1 (ko) | 2006-04-13 | 2014-04-28 | 다이호야쿠힌고교 가부시키가이샤 | 염증성 장질환 치료제 |
| TWI426909B (zh) | 2006-06-30 | 2014-02-21 | Taiho Pharmaceutical Co Ltd | Radiation therapy enhancer |
| CN104395307A (zh) * | 2013-06-17 | 2015-03-04 | 大鹏药品工业株式会社 | 地匹福林盐酸盐的稳定型晶体及其结晶化方法 |
| CN103613877B (zh) * | 2013-11-20 | 2017-09-19 | 上海锦湖日丽塑料有限公司 | 适于吹塑成型的高耐热abs树脂组合物及其制备方法 |
| CN104744443A (zh) | 2013-12-26 | 2015-07-01 | 江苏豪森药业股份有限公司 | 嘧啶二酮类化合物盐酸盐新晶型及其制备方法 |
| CN103788075B (zh) * | 2014-02-19 | 2018-03-27 | 齐鲁制药有限公司 | 一种胸苷磷酸化酶抑制剂的结晶形式及其制备方法 |
| CN104945384B (zh) | 2014-03-25 | 2018-10-16 | 江苏豪森药业集团有限公司 | 5-氯-6-[(2-亚氨基-1-吡咯烷)甲基]-2,4(1h,3h)-嘧啶二酮或其盐的制备方法 |
| CN104945385A (zh) | 2014-03-31 | 2015-09-30 | 江苏豪森药业股份有限公司 | Tipracil盐酸盐的新晶型及其制备方法 |
| CN103980253B (zh) | 2014-05-06 | 2015-07-08 | 济南百诺医药科技开发有限公司 | 一种5-氯-6-(2-亚氨基吡咯烷基-1-基)甲基-2,4-(1h, 3h)嘧啶二酮盐酸盐的合成方法 |
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2014
- 2014-06-17 CN CN201480000562.4A patent/CN104395307A/zh active Pending
- 2014-06-17 US US14/896,748 patent/US9527833B2/en active Active
- 2014-06-17 PT PT148143548T patent/PT3012255T/pt unknown
- 2014-06-17 JP JP2015522923A patent/JP6364409B2/ja active Active
- 2014-06-17 SI SI201431915T patent/SI3012255T1/sl unknown
- 2014-06-17 CN CN201910933531.9A patent/CN110746403A/zh active Pending
- 2014-06-17 NZ NZ714090A patent/NZ714090A/en unknown
- 2014-06-17 SG SG11201509189SA patent/SG11201509189SA/en unknown
- 2014-06-17 EP EP14814354.8A patent/EP3012255B1/fr active Active
- 2014-06-17 ES ES14814354T patent/ES2898408T3/es active Active
- 2014-06-17 GE GEAP201414034A patent/GEP20186875B/en unknown
- 2014-06-17 EP EP17204730.0A patent/EP3305779A1/fr active Pending
- 2014-06-17 RS RS20211505A patent/RS62691B1/sr unknown
- 2014-06-17 SG SG10201710916YA patent/SG10201710916YA/en unknown
- 2014-06-17 MX MX2015016986A patent/MX2015016986A/es active IP Right Grant
- 2014-06-17 RU RU2017124790A patent/RU2674441C1/ru active
- 2014-06-17 BR BR112015031619-0A patent/BR112015031619B1/pt active IP Right Grant
- 2014-06-17 DK DK14814354.8T patent/DK3012255T3/da active
- 2014-06-17 TW TW103120948A patent/TWI639592B/zh active
- 2014-06-17 PL PL14814354T patent/PL3012255T3/pl unknown
- 2014-06-17 CN CN201910111208.3A patent/CN109912573A/zh active Pending
- 2014-06-17 CN CN201610818347.6A patent/CN106967051A/zh active Pending
- 2014-06-17 MY MYPI2015002887A patent/MY173410A/en unknown
- 2014-06-17 RU RU2016100972A patent/RU2640417C2/ru active
- 2014-06-17 MA MA38668A patent/MA38668B2/fr unknown
- 2014-06-17 KR KR1020167001279A patent/KR101806346B1/ko active IP Right Grant
- 2014-06-17 CA CA2985006A patent/CA2985006C/fr active Active
- 2014-06-17 UA UAA201600333A patent/UA112626C2/uk unknown
- 2014-06-17 HU HUE14814354A patent/HUE057352T2/hu unknown
- 2014-06-17 AU AU2014282281A patent/AU2014282281C1/en active Active
- 2014-06-17 CA CA2914999A patent/CA2914999C/fr active Active
- 2014-06-17 GE GEAP201414225A patent/GEP20186841B/en unknown
- 2014-06-17 HR HRP20211903TT patent/HRP20211903T1/hr unknown
- 2014-06-17 LT LTEPPCT/JP2014/065985T patent/LT3012255T/lt unknown
- 2014-06-17 WO PCT/JP2014/065985 patent/WO2014203877A1/fr active Application Filing
- 2014-06-17 SG SG10202007643SA patent/SG10202007643SA/en unknown
- 2014-06-17 SG SG10201912293UA patent/SG10201912293UA/en unknown
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2015
- 2015-04-10 HK HK15103542.0A patent/HK1203071A1/xx unknown
- 2015-12-17 PH PH12015502809A patent/PH12015502809A1/en unknown
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2016
- 2016-11-16 US US15/352,858 patent/US10138223B2/en active Active
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2018
- 2018-05-02 US US15/969,434 patent/US10457666B2/en active Active
- 2018-07-02 JP JP2018126102A patent/JP6526883B2/ja active Active
- 2018-08-20 AU AU2018219967A patent/AU2018219967C1/en active Active
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2021
- 2021-12-07 CY CY20211101073T patent/CY1124868T1/el unknown
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